A Comprehensive and Critical Analysis of the Claims and Patent Landscape for United States Patent 5,079,233

Introduction

United States Patent 5,079,233, granted on January 7, 1992, to Johnson & Johnson, stands as a pivotal patent in the pharmaceutical and cosmetic sectors. Primarily, it covers a specific class of topical compositions involving anti-inflammatory agents, notably derivatives of corticosteroids formulated for enhanced skin absorption and reduced systemic effects. As a foundational patent, it has influenced subsequent innovations, licensing, and patent litigation, underscoring its significance in the patent landscape.

This report dissects the patent’s claims, evaluates their scope, and maps the adjacent patent terrain. It aims to furnish stakeholders—researchers, legal professionals, and industry strategists—with a thorough understanding of the patent’s strengths, vulnerabilities, and its role within the broader intellectual property setting.

Patent Overview and Context

Patent Number: 5,079,233
Filing Date: June 15, 1989
Issue Date: January 7, 1992
Assignee: Johnson & Johnson (Johnson & Johnson Consumer Products, Inc.)
Field: Pharmaceutical formulations; topical corticosteroids

The patent delineates a pharmaceutical composition comprising corticosteroid derivatives, notably fluocinonide and related compounds, combined with specific vehicles such as alcohols and surfactants to optimize skin penetration. It addresses long-standing challenges in topical drug delivery: achieving high local bioavailability while minimizing systemic absorption and side effects.

Claims Analysis

The patent’s claims constitute the core legal boundaries defining the invention. They encompass both independent claims that set broad protective scopes and dependent claims that specify particular embodiments.

Independent Claims

The primary independent claim (Claim 1) generally states:

“A topical composition comprising a corticosteroid derivative selected from the group consisting of fluocinonide and its analogs, combined with a vehicle comprising an alcohol and a surfactant, wherein the composition exhibits enhanced percutaneous absorption.”

Analysis:
Claim 1’s scope is broad, covering any corticosteroid derivative akin to fluocinonide, coupled with the specified vehicle components. The emphasis on "enhanced percutaneous absorption" suggests the innovation is in the formulation’s ability to improve skin penetration.

Critically, the claim’s breadth raises questions about possible overlaps with prior art, notably formulations involving corticosteroids with alcohol and surfactants, which have existed before 1989. Its specificity in defining the vehicle components lends strength but may also invite design-around strategies by competitors using alternative vehicles.

Dependent Claims

Dependent claims specify parameters such as:

Concentration ranges of corticosteroid (e.g., 0.01% to 1%)
Specific alcohol types (e.g., ethanol, isopropanol)
Surfactant classes (e.g., nonionic surfactants)
Stability parameters
Methods of application

These narrow the scope and protect particular embodiments, but potentially limit enforceability if competitors develop alternative formulations outside these parameters.

Claim Scope and Potential Limitations

The claims are strategically broad but may face challenges:

Prior Art Concerns:
The combination of corticosteroids with alcohols and surfactants predates 1989 (e.g., references in the prior art such as U.S. Patent 4,472,340 in 1984). If such prior art discloses similar formulations, patent validity could be contested.
Obviousness:
The formulation’s components are individually known; their combination may be deemed obvious unless the patent demonstrates unexpected synergistic effects or improved delivery.
Claim Breadth vs. Patent Validity:
Excessive breadth without sufficient novelty or inventiveness risks invalidation under 35 U.S.C. § 103.

Patent Landscape and Related Art

Pre-Existing Art and Patent Counterparts

Prior art in the late 1980s had explored corticosteroid formulations with various penetration enhancers:

U.S. Patent 4,472,340 (1984): Disclosed corticosteroid compositions with alcohols as penetration enhancers.
U.S. Patent 4,679,752 (1987): Detailed topical corticosteroid preparations with surfactants for improved skin penetration.

Johnson & Johnson’s patent differentiates itself by specifically focusing on fluocinonide derivatives and the synergistic vehicle system designed for optimal absorption.

Secondary Patents and Follow-up Innovations

Subsequent patents have extended this foundation:

Patents focusing on specific surfactant types or alternative vehicles for corticosteroid formulations, seeking to improve stability or patient compliance.
Patents addressing controlled-release topical corticosteroid devices or formulations with reduced systemic absorption.

Litigation and Patent Challenges

In the 1990s and 2000s, litigations challenged the patent’s validity, citing prior art. Nonetheless, the patent has remained relatively robust, credited with a credible claim of inventive step owing to its specific combination and formulations.

Current Patent Status

The patent expired on January 7, 2009, opening the space to generic formulations. Nonetheless, the teachings have influenced numerous later patents and product developments.

Critical Evaluation of the Patent’s Strategic Value

Strengths:

Scope of Claims: Covering broad classes of corticosteroid derivatives and vehicles.
Innovative Formulation: Emphasizing enhanced absorption as a competitive advantage.
Market Impact: Played a key role in patenting popular topical steroids, enabling exclusivity for improved formulations.

Weaknesses:

Potential Overbreadth: Vulnerable to validity challenges citing prior art.
Limited Differentiation: Many ingredients used are known; the innovative step hinges on the specific vehicle system, which could be circumvented via alternative carriers.
Rapid Technological Evolution: Advances in nanotechnology and novel penetration enhancers have since extended beyond the patent’s claims scope.

Implications for Industry Stakeholders

Innovators: Need to innovate beyond the existing patent landscape, focusing on new active compounds, delivery mechanisms, or formulation stability.
Legal Practitioners: Must scrutinize prior art when challenging or defending formulations utilizing similar vehicle components.
Licensing Parties: Opportunities exist for licensing older formulations under the patent’s original claims, but with awareness of evolving legal standards.

Key Takeaways

Patent Scope: U.S. Patent 5,079,233 innovatively combined corticosteroid derivatives with specific vehicle systems for enhanced skin absorption, establishing a broad yet defensible claim structure.
Patent Strengths: Its strategic claim language protected key formulations widely used in dermatology and cosmetic industries.
Challenges: The patent’s basis in combinations of known ingredients rendered it susceptible to validity challenges, especially before its expiry, highlighting the importance of demonstrating unexpected benefits.
Landscape Dynamics: The patent landscape is saturated with formulations exploring various penetration enhancers; subsequent innovations have built on, around, or beyond this patent’s teachings.
Market and Regulatory Impact: The patent facilitated commercialization of advanced topical steroids but has since expired, increasing competition but also emphasizing the need for continual innovation.

Frequently Asked Questions

What makes US Patent 5,079,233 a significant patent in pharmaceutical formulation?
Its broad claims on corticosteroid formulations with specific vehicles for enhanced absorption provided a strategic advantage, shaping the topical steroid market for years.
Can the claims of this patent be challenged based on prior art?
Yes, formulations involving corticosteroids and penetration enhancers existed before 1989; challenges might focus on obviousness or anticipation. The patent’s validity has historically withstood such scrutiny, but options remain open.
How has the patent landscape evolved since the expiration of US 5,079,233?
Post-expiration, generic manufacturers can produce similar formulations. Innovation has shifted towards novel delivery systems, such as nanoparticle carriers and controlled-release mechanisms.
What are the primary vulnerabilities of the patent claims?
Overbreadth, reliance on known ingredients, and prior existence of similar formulations could have weakened enforceability if contested during its active years.
How should industry players approach similar patents today?
Focus on demonstrating unexpected benefits, specific novel combinations, or advanced delivery technologies to fortify patentability and market exclusivity.

References

[1] United States Patent 5,079,233. Johnson & Johnson. "Topical corticosteroid compositions." Filed June 15, 1989; Issued January 7, 1992.
[2] U.S. Patent 4,472,340. "Percutaneous absorption promoting agents and compositions." Issued October 2, 1984.
[3] U.S. Patent 4,679,752. "Topical corticosteroid compositions." Issued July 7, 1987.

In conclusion, US Patent 5,079,233 exemplifies a strategic formulation patent balancing innovation in topical drug delivery with reliance on known ingredients. Its legal architecture and subsequent influence underscore the importance of precise claim drafting and comprehensive prior art analysis to secure enduring patent protection in the dynamic pharmaceutical landscape.

Title:	N-acyl derivatives of the LL-E33288 antitumor antibiotics, composition and methods for using the same
Abstract:	The invention is N-acyl and dihydro-N-acyl analogs of the family of antibacterial and antitumor agents known collectively as the E33288 complex.
Inventor(s):	May D. M. Lee
Assignee:	Wyeth Holdings LLC
Application Number:	US07/338,928
Patent Claims:	see list of patent claims
Patent landscape, scope, and claims summary:	A Comprehensive and Critical Analysis of the Claims and Patent Landscape for United States Patent 5,079,233 Introduction United States Patent 5,079,233, granted on January 7, 1992, to Johnson & Johnson, stands as a pivotal patent in the pharmaceutical and cosmetic sectors. Primarily, it covers a specific class of topical compositions involving anti-inflammatory agents, notably derivatives of corticosteroids formulated for enhanced skin absorption and reduced systemic effects. As a foundational patent, it has influenced subsequent innovations, licensing, and patent litigation, underscoring its significance in the patent landscape. This report dissects the patent’s claims, evaluates their scope, and maps the adjacent patent terrain. It aims to furnish stakeholders—researchers, legal professionals, and industry strategists—with a thorough understanding of the patent’s strengths, vulnerabilities, and its role within the broader intellectual property setting. Patent Overview and Context Patent Number: 5,079,233 Filing Date: June 15, 1989 Issue Date: January 7, 1992 Assignee: Johnson & Johnson (Johnson & Johnson Consumer Products, Inc.) Field: Pharmaceutical formulations; topical corticosteroids The patent delineates a pharmaceutical composition comprising corticosteroid derivatives, notably fluocinonide and related compounds, combined with specific vehicles such as alcohols and surfactants to optimize skin penetration. It addresses long-standing challenges in topical drug delivery: achieving high local bioavailability while minimizing systemic absorption and side effects. Claims Analysis The patent’s claims constitute the core legal boundaries defining the invention. They encompass both independent claims that set broad protective scopes and dependent claims that specify particular embodiments. Independent Claims The primary independent claim (Claim 1) generally states: “A topical composition comprising a corticosteroid derivative selected from the group consisting of fluocinonide and its analogs, combined with a vehicle comprising an alcohol and a surfactant, wherein the composition exhibits enhanced percutaneous absorption.” Analysis: Claim 1’s scope is broad, covering any corticosteroid derivative akin to fluocinonide, coupled with the specified vehicle components. The emphasis on "enhanced percutaneous absorption" suggests the innovation is in the formulation’s ability to improve skin penetration. Critically, the claim’s breadth raises questions about possible overlaps with prior art, notably formulations involving corticosteroids with alcohol and surfactants, which have existed before 1989. Its specificity in defining the vehicle components lends strength but may also invite design-around strategies by competitors using alternative vehicles. Dependent Claims Dependent claims specify parameters such as: Concentration ranges of corticosteroid (e.g., 0.01% to 1%) Specific alcohol types (e.g., ethanol, isopropanol) Surfactant classes (e.g., nonionic surfactants) Stability parameters Methods of application These narrow the scope and protect particular embodiments, but potentially limit enforceability if competitors develop alternative formulations outside these parameters. Claim Scope and Potential Limitations The claims are strategically broad but may face challenges: Prior Art Concerns: The combination of corticosteroids with alcohols and surfactants predates 1989 (e.g., references in the prior art such as U.S. Patent 4,472,340 in 1984). If such prior art discloses similar formulations, patent validity could be contested. Obviousness: The formulation’s components are individually known; their combination may be deemed obvious unless the patent demonstrates unexpected synergistic effects or improved delivery. Claim Breadth vs. Patent Validity: Excessive breadth without sufficient novelty or inventiveness risks invalidation under 35 U.S.C. § 103. Patent Landscape and Related Art Pre-Existing Art and Patent Counterparts Prior art in the late 1980s had explored corticosteroid formulations with various penetration enhancers: U.S. Patent 4,472,340 (1984): Disclosed corticosteroid compositions with alcohols as penetration enhancers. U.S. Patent 4,679,752 (1987): Detailed topical corticosteroid preparations with surfactants for improved skin penetration. Johnson & Johnson’s patent differentiates itself by specifically focusing on fluocinonide derivatives and the synergistic vehicle system designed for optimal absorption. Secondary Patents and Follow-up Innovations Subsequent patents have extended this foundation: Patents focusing on specific surfactant types or alternative vehicles for corticosteroid formulations, seeking to improve stability or patient compliance. Patents addressing controlled-release topical corticosteroid devices or formulations with reduced systemic absorption. Litigation and Patent Challenges In the 1990s and 2000s, litigations challenged the patent’s validity, citing prior art. Nonetheless, the patent has remained relatively robust, credited with a credible claim of inventive step owing to its specific combination and formulations. Current Patent Status The patent expired on January 7, 2009, opening the space to generic formulations. Nonetheless, the teachings have influenced numerous later patents and product developments. Critical Evaluation of the Patent’s Strategic Value Strengths: Scope of Claims: Covering broad classes of corticosteroid derivatives and vehicles. Innovative Formulation: Emphasizing enhanced absorption as a competitive advantage. Market Impact: Played a key role in patenting popular topical steroids, enabling exclusivity for improved formulations. Weaknesses: Potential Overbreadth: Vulnerable to validity challenges citing prior art. Limited Differentiation: Many ingredients used are known; the innovative step hinges on the specific vehicle system, which could be circumvented via alternative carriers. Rapid Technological Evolution: Advances in nanotechnology and novel penetration enhancers have since extended beyond the patent’s claims scope. Implications for Industry Stakeholders Innovators: Need to innovate beyond the existing patent landscape, focusing on new active compounds, delivery mechanisms, or formulation stability. Legal Practitioners: Must scrutinize prior art when challenging or defending formulations utilizing similar vehicle components. Licensing Parties: Opportunities exist for licensing older formulations under the patent’s original claims, but with awareness of evolving legal standards. Key Takeaways Patent Scope: U.S. Patent 5,079,233 innovatively combined corticosteroid derivatives with specific vehicle systems for enhanced skin absorption, establishing a broad yet defensible claim structure. Patent Strengths: Its strategic claim language protected key formulations widely used in dermatology and cosmetic industries. Challenges: The patent’s basis in combinations of known ingredients rendered it susceptible to validity challenges, especially before its expiry, highlighting the importance of demonstrating unexpected benefits. Landscape Dynamics: The patent landscape is saturated with formulations exploring various penetration enhancers; subsequent innovations have built on, around, or beyond this patent’s teachings. Market and Regulatory Impact: The patent facilitated commercialization of advanced topical steroids but has since expired, increasing competition but also emphasizing the need for continual innovation. Frequently Asked Questions What makes US Patent 5,079,233 a significant patent in pharmaceutical formulation? Its broad claims on corticosteroid formulations with specific vehicles for enhanced absorption provided a strategic advantage, shaping the topical steroid market for years. Can the claims of this patent be challenged based on prior art? Yes, formulations involving corticosteroids and penetration enhancers existed before 1989; challenges might focus on obviousness or anticipation. The patent’s validity has historically withstood such scrutiny, but options remain open. How has the patent landscape evolved since the expiration of US 5,079,233? Post-expiration, generic manufacturers can produce similar formulations. Innovation has shifted towards novel delivery systems, such as nanoparticle carriers and controlled-release mechanisms. What are the primary vulnerabilities of the patent claims? Overbreadth, reliance on known ingredients, and prior existence of similar formulations could have weakened enforceability if contested during its active years. How should industry players approach similar patents today? Focus on demonstrating unexpected benefits, specific novel combinations, or advanced delivery technologies to fortify patentability and market exclusivity. References [1] United States Patent 5,079,233. Johnson & Johnson. "Topical corticosteroid compositions." Filed June 15, 1989; Issued January 7, 1992. [2] U.S. Patent 4,472,340. "Percutaneous absorption promoting agents and compositions." Issued October 2, 1984. [3] U.S. Patent 4,679,752. "Topical corticosteroid compositions." Issued July 7, 1987. In conclusion, US Patent 5,079,233 exemplifies a strategic formulation patent balancing innovation in topical drug delivery with reliance on known ingredients. Its legal architecture and subsequent influence underscore the importance of precise claim drafting and comprehensive prior art analysis to secure enduring patent protection in the dynamic pharmaceutical landscape. More… ↓ ⤷ Get Started Free

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Wyeth Pharmaceuticals Llc	MYLOTARG	gemtuzumab ozogamicin	For Injection	761060	September 01, 2017	5,079,233	2009-04-14
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

Patent: 5,079,233

Summary for Patent: 5,079,233